YM 298198 hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 2448 - YM 298198 hydrochloride | C18H22N4OS.HCl | CAS No. 1216398-09-2
Description: Highly potent, selective non-competitive mGlu1 antagonist
Chemical Name: 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM); inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively), and is orally active in vivo, demonstrating an antinociceptive effect in hyperalgesic mice. Desmethyl derivative (Cat. No. 2447) also available.

Licensing Information

Sold with the permission of Astellas Pharma Inc.

Technical Data

M. Wt 378.92
Formula C18H22N4OS.HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 1216398-09-2
PubChem ID 45073464
InChI Key WYTJVUVCSUWZTH-UHFFFAOYSA-N
Smiles Cl.CN(C1CCCCC1)C(=O)C1=C(C)N2C(S1)=NC1=CC=C(N)C=C21

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 37.89 100

Preparing Stock Solutions

The following data is based on the product molecular weight 378.92. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.64 mL 13.2 mL 26.39 mL
5 mM 0.53 mL 2.64 mL 5.28 mL
10 mM 0.26 mL 1.32 mL 2.64 mL
50 mM 0.05 mL 0.26 mL 0.53 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Kohara et al (2005) Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective and noncompetitive antagonist of metabo J.Pharmacol.Exp.Ther. 315 163 PMID: 15976016

Emery et al (2010) The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation. J.Biol.Chem. 285 26041 PMID: 20566651


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Citations for YM 298198 hydrochloride

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